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Avanafil

阿伐那非,阿伐那菲

Avanafil是一种高度选择性PDE5抑制剂，IC50为1nM.

目录号
EY0305
EY0305
EY0305
纯度
99.68%
99.68%
99.68%
规格
50 mg
100 mg
500 mg
原价
515
890
3100
售价
515
890
3100
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    1-300微克/千克十二指肠治疗或静脉注射。

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Soliman KA, Ibrahim HK, Ghorab MM. Effects of different combinations of nanocrystallization technologies on avanafil nanoparticles: in vitro, in vivo and stability evaluation. Int J Pharm. 2017 Jan 30;517(1-2):148-156. doi: 10.1016/j.ijpharm.2016.12.012.
    [2] Soliman KA, Ibrahim HK, Ghorab MM. Formulation of avanafil in a solid self-nanoemulsifying drug delivery system for enhanced oral delivery. Eur J Pharm Sci. 2016 Oct 10;93:447-55. doi: 10.1016/j.ejps.2016.08.050.
    [3] Soliman KA, Ibrahim HK, Ghorab MM. Effect of different polymers on avanafil-β-cyclodextrin inclusion complex: in vitro and in vivo evaluation. Int J Pharm. 2016 Oct 15;512(1):168-77. doi: 10.1016/j.ijpharm.2016.08.044.

    分子式
    C23H26ClN7O3    		 分子量
    483.95    		 CAS号
    330784-47-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    97 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT01054430 Erectile Dysfunction Drug: avanafil VIVUS, Inc. Phase 1 2010-01-01 2011-01-05
    NCT01095601 Healthy Drug: Avanafil VIVUS, Inc. Phase 1 2010-04-01 2011-01-05
    NCT01054261 Renal Drug: avanafil VIVUS, Inc. Phase 1 2010-01-01 2011-01-05
    NCT00853606 Erectile Dysfunction Drug: avanafil VIVUS, Inc. Phase 3 2009-03-01 2012-08-10
    NCT01117038 Erectile Dysfunction Drug: avanafil and enalapril|Drug: avanafil and amlodipine VIVUS, Inc. Phase 1 2010-04-01 2011-08-09
    NCT02477436 Erectile Dysfunction Drug: Avanafil|Drug: Placebo Pusan National University Hospital Phase 2 2008-02-01 2015-06-23
    NCT01100021 Erectile Dysfunction Drug: Tamsulosin and avanafil|Drug: Doxazosin and avanafil VIVUS, Inc. Phase 1 2010-02-01 2011-01-05
    NCT01768676 Erectile Dysfunction Drug: avanafil|Drug: Placebo VIVUS, Inc. Phase 4 2012-12-01 2015-11-05
    NCT01705197 Erectile Dysfunction Drug: Avanafil 100 or 200mg JW Pharmaceutical Phase 3 2012-02-01 2017-03-08
    NCT01095588 Erectile Dysfunction Drug: 200 mg Avanafil|Drug: Placebo VIVUS, Inc. Phase 1 2010-04-01 2011-01-05
    NCT02033200 Vision Drug: Stendra 200 mg|Drug: Placebo VIVUS, Inc. Phase 4 2014-01-01 2015-03-02
    NCT00903981 Erectile Dysfunction Drug: Avanafil|Drug: Avanafil|Drug: Placebo JW Pharmaceutical Phase 3 2009-03-01 2010-04-22
    NCT01054859 Erectile Dysfunction Drug: avanafil|Other: alcohol|Drug: avanafil VIVUS, Inc. Phase 1 2010-01-01 2011-01-05
    NCT00769041 Erectile Dysfunction Drug: moxifloxacin|Drug: avanafil|Drug: avanafil|Drug: sugar pill VIVUS, Inc.|Covance Phase 1 2008-10-01 2011-01-05
    NCT00770042 Erectile Dysfunction Drug: Ritonavir|Drug: Ketoconazole|Drug: Erythomycin|Drug: Avanafil|Drug: Avanafil|Drug: Avanafil VIVUS, Inc. Phase 1 2008-10-01 2009-11-30
    NCT02503306 Sexual Function and Fertility Disorders NEC-Erectile Dysfunction Drug: AVANAFIL|Drug: placebo Sanofi Phase 3 2015-07-01 2016-03-16
    NCT00809471 Erectile Dysfunction Drug: placebo|Drug: avanafil|Drug: avanafil VIVUS, Inc. Phase 3 2008-12-01 2012-08-10
    NCT00895011 Erectile Dysfunction Drug: Placebo|Drug: Avanafil|Drug: Avanafil VIVUS, Inc. Phase 3 2009-04-01 2012-09-14
    NCT00914511 Avanfil ADME|Semen Exposure|Sperm Function Drug: avanafil 200mg|Drug: avanafil 200mg VIVUS, Inc. Phase 1 2009-05-01 2011-01-05
    NCT00790751 Erectile Dysfunction Drug: placebo|Drug: avanafil|Drug: avanafil|Drug: avanafil VIVUS, Inc. Phase 3 2008-11-01 2012-06-27
    NCT01415128 Erectile Dysfunction Drug: Omeprazole|Drug: Rosiglitazone|Drug: Desipramine VIVUS, Inc. Phase 1 2010-04-01 2011-08-10
    NCT01698684 Erectile Dysfunction Drug: Placebo|Drug: Avanafil 100 mg|Drug: Avanafil 200 mg VIVUS, Inc. Phase 4 2012-09-01 2014-10-21
    NCT02757807 Erectile Dysfunction Behavioral: Utilization of Serenita for Relaxation Eco Fusion 2016-07-01 2016-07-19

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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